正交试验优选尼古丁-β-环糊精包合物的制备工艺及质量考察

Optimization of the Preparation Technology of Nicotine-β-cyclodextrin Inclusion Compound by Orthogonal Test and Quality Evaluation

目的:优化尼古丁-β环糊精包合物的制备工艺,并评价其质量。方法:采用饱和水溶液法制备尼古丁β-环糊精包合物,利用正交试验法,选取尼古丁与β-环糊精的配比(A)、包合温度(B)、包合时间(C)为因素,以包合率和收率为指标优选包合物最佳制备工艺,采用包合平衡常数法验证包合物的形成并考察包合物体外溶出特性。分别对尼古丁β-环糊精包合物及其混合物进行高温、高湿和强光试验,考察其稳定性。结果:最佳包合条件A为1:3,B为60℃,C为2 h,包合率达65.28%,收率为79.55%。150 min缓慢释药量达92.26%。在不同温度、湿度和强光条件下,包合物中尼古丁的含量均显著高于混合物。结论:所选制备工艺简单且条件易于控制,所制包合物稳定性良好且具有缓释作用。

OBJECTIVE： To prepare nicotine-β- CD inclusion compound and evaluate its quality. METHODS： The inclusion complex was prepared by saturated water solution method, and the preparation conditions were optimized by orthogonal test with the ratio of nicotine to β-CD （A）, the inclusion temperature （B）, the inclusion time （C） as factors and with the inclusion rate and the yield as indexes for evaluation. The formation of the inclusion complexes were verified by inclusion equilibrium constant analysis and its dissolution characteristics in vitro were investigated. The stability of nicotine - β - CD inclusion compound and the mixture of nicotine and 13 - CD were studied by conducting high - temperature, high humidity and high light tests. RESULTS： The optimum preparation conditions for the inclusion compound were established as： A was 1 ： 3, B was 60 ℃ and C was 2 hours. The inclusion rate of nicotine reached 65.28%; the yield was 79.55%, and the slow-release rate at 150 min was 92.26%. Under different temperature, humidity and high light conditions, the content of nicotine was always significantly higher in the inclusion complex than in the mixture. CONCLUSIONS： The inclusion technology is simple and the conditions were easily controllable, and the prepared nicotine-β- CD inclusion compound enjoys good stability and sustained - release property.